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Unprecedented Discovery of novel small molecule that target six drug targets upregulated in cancers

Raafat ElAwady,1,2 Dr Srinivasulu Vunnam,1 Cijo George Vazhappilly,1 Taleb H. AL-Tel*1,2 1Sharjah Institute for Medical Research and 2College of Pharmacy University of Sharjah, Sharjah, 27272 UAE This invention describes novel heterocyclic systems, which possess many biological activities including but not limited to, anticancer activity and are useful in the treatment of many disease states related to cell proliferation. In particular, new pyran derivatives are provided having the general formula A and B, processes for their preparation, and methods for their pharmaceutical applications for example here as anticancer agents. These compounds were found to have antiproliferative effects against multiple cancer cell lines and showed considerably less toxicity to normal fibroblasts. These compounds exhibited typical anticancer properties by inducing caspase-mediated cell death mechanisms and arresting cancer cell progression. Further, these novel compounds were able to target multiple key proteins/enzymes, including thioredoxin reductase, glutathione reductase, transferrin receptors, inisitol-3-phosphate synthase, cystolic aminopeptidase and transketolase that are over-expressed in tumor cells, which may facilitate to address the current issues in therapy such as multi-drug resistance and/or tumor relapse.


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